AU2012335714B2 - Modulators of ATP-binding cassette transporters - Google Patents

Modulators of ATP-binding cassette transporters Download PDF

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Publication number
AU2012335714B2
AU2012335714B2 AU2012335714A AU2012335714A AU2012335714B2 AU 2012335714 B2 AU2012335714 B2 AU 2012335714B2 AU 2012335714 A AU2012335714 A AU 2012335714A AU 2012335714 A AU2012335714 A AU 2012335714A AU 2012335714 B2 AU2012335714 B2 AU 2012335714B2
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Prior art keywords
compound
formula
disease
vol
cftr
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AU2012335714A1 (en
Inventor
Anusuya Choudhury
Cristian L. Harrison
Licong JIANG
Benjamin Joseph Littler
Adam Looker
Eduard LUSS-LUSIS
Michael P. Ryan
Ravikanth VELURI
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Endocrinology (AREA)
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  • Dermatology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2012335714A 2011-11-08 2012-11-08 Modulators of ATP-binding cassette transporters Active AU2012335714B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201161557043P 2011-11-08 2011-11-08
US61/557,043 2011-11-08
US201261610257P 2012-03-13 2012-03-13
US61/610,257 2012-03-13
PCT/US2012/064217 WO2013070961A1 (en) 2011-11-08 2012-11-08 Modulators of atp-binding cassette transporters

Publications (2)

Publication Number Publication Date
AU2012335714A1 AU2012335714A1 (en) 2014-05-22
AU2012335714B2 true AU2012335714B2 (en) 2017-04-13

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AU2012335714A Active AU2012335714B2 (en) 2011-11-08 2012-11-08 Modulators of ATP-binding cassette transporters

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US (1) US9254291B2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
EP (1) EP2776427B1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
JP (1) JP6072056B2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
KR (1) KR101985044B1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
CN (1) CN104039775B (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
AU (1) AU2012335714B2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
CA (1) CA2852991C (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
ES (1) ES2622154T3 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
HR (1) HRP20170458T1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
IL (1) IL232308A (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
IN (1) IN2014KN00885A (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
LT (1) LT2776427T (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
ME (1) ME02650B (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
MX (1) MX357328B (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
RU (1) RU2640420C2 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
SI (1) SI2776427T1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
WO (1) WO2013070961A1 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)
ZA (1) ZA201403262B (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html)

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CA2537841A1 (en) 2003-09-06 2005-03-24 Vertex Pharmaceuticals Incorporated Modulators of atp-binding cassette transporters
US7977322B2 (en) 2004-08-20 2011-07-12 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
WO2007056341A1 (en) 2005-11-08 2007-05-18 Vertex Pharmaceuticals Incorporated Heterocyclic modulators of atp-binding cassette transporters
EP2532650A3 (en) 2004-06-24 2013-11-06 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
MX2008002019A (es) 2005-08-11 2008-04-16 Vertex Pharma Moduladores del regulador de conductancia transmembrana de fibrosis quistica.
EP2016065B1 (en) 2005-12-28 2012-09-19 Vertex Pharmaceuticals Incorporated 1-(benzo[d][1,3]dioxol-5-yl)-n-(phenyl)cyclopropane-carboxamide derivatives and related compounds as modulators of atp-binding cassette transporters for the treatment of cystic fibrosis
EP3219705B1 (en) 2005-12-28 2020-03-11 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
USRE50453E1 (en) 2006-04-07 2025-06-10 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US7645789B2 (en) 2006-04-07 2010-01-12 Vertex Pharmaceuticals Incorporated Indole derivatives as CFTR modulators
US10022352B2 (en) 2006-04-07 2018-07-17 Vertex Pharmaceuticals Incorporated Modulators of ATP-binding cassette transporters
ES2659364T3 (es) 2006-04-07 2018-03-15 Vertex Pharmaceuticals Incorporated Moduladores de transportadores del casete de unión a ATP
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
NZ581259A (en) 2007-05-09 2012-07-27 Vertex Pharma Modulators of cystic fibrosis transmembrane conductance regulator
JP5389030B2 (ja) 2007-08-24 2014-01-15 バーテックス ファーマシューティカルズ インコーポレイテッド （特に）嚢胞性線維症の処置に有用なイソチアゾロピリジノン
SI2578571T1 (sl) 2007-11-16 2016-01-29 Vertex Pharmaceuticals Incorporated Izokinolinski modulatorji prenašalcev z atp-vezavno kaseto
US20100036130A1 (en) 2007-12-07 2010-02-11 Vertex Pharmaceuticals Incorporated Processes for producing cycloalkylcarboxamido-pyridine benzoic acids
PT2639223T (pt) 2007-12-07 2017-05-08 Vertex Pharma Processos para produção de ácidos cicloalquilcarboxamido-piridinabenzoicos
WO2009073757A1 (en) 2007-12-07 2009-06-11 Vertex Pharmaceuticals Incorporated Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid
CA2708146A1 (en) * 2007-12-07 2009-06-18 Vertex Pharmaceuticals Incorporated Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid
CN102245573B (zh) 2008-02-28 2013-11-20 沃泰克斯药物股份有限公司 作为cftr调节剂的杂芳基衍生物
EP2615085B1 (en) 2008-03-31 2015-08-26 Vertex Pharmaceuticals Incorporated Pyridyl derivatives as CFTR modulators
CN102164587A (zh) 2008-09-29 2011-08-24 沃泰克斯药物股份有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]间二氧杂环戊烯-5-基)环丙烷甲酰氨基)-3-甲基吡啶-2-基)苯甲酸的剂量单元
NO2821400T3 (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html) 2009-03-20 2018-02-24
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
CN102917692A (zh) 2010-04-07 2013-02-06 弗特克斯药品有限公司 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的药物组合物和其给药方法
ES2579965T3 (es) 2010-04-07 2016-08-17 Vertex Pharmaceuticals Incorporated Las formas sólidas de 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-il) Ciclopropano carboxamida)-3-metilpiridin-2-il)benzoico
SG184987A1 (en) * 2010-04-22 2012-11-29 Vertex Pharma Process of producing cycloalkylcarboxamido-indole compounds
RU2640420C2 (ru) 2011-11-08 2018-01-09 Вертекс Фармасьютикалз Инкорпорейтед Модуляторы транспортеров атф-связывающей кассеты
US20130224293A1 (en) 2012-02-27 2013-08-29 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
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ES2622154T3 (es) 2017-07-05
SI2776427T1 (sl) 2017-05-31
MX357328B (es) 2018-07-05
IL232308A (en) 2016-11-30
JP2014534236A (ja) 2014-12-18
IN2014KN00885A (c_deeref_Disk_and_Scratch_Disk_Pools_and_Their_Defaults.html) 2015-10-02

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